Numerous naturally occurring tumor inhibitors have been discovered over the past several years and, while these compounds are potential candidates for clinical use in the management of neoplastic diseases, they also represent new chemical structures which can be used as "templates" in the design of new synthetic agents with potential antineoplastic activity. During the course of our research for new "lead compounds" which possess antineoplastic activity we prepare derivatives of acylated 2,3-dihydro-5-phenyl-6,7-bis (hydroxymethyl)-1H-pyrrolozines. The significant reproducible antileukemic activity shown by these compounds, and related pyrrole derivatives, has formed the basis for additional studies with this broad class of compounds. The research will use cluster analysis methods to design new series of compounds, quantitative structure-activity relationship studies to evaluate the antineoplastic activity data, and biochemical studies (DNA intercalation and effects on DNA, RNA, and protein synthesis) to point to mechanisms of action.